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Submit ReviewLY 320135 is a potent CB1 receptor antagonist/inverse agonist (Ki = 141 nM) with greater than 70-fold selectivity over CB2 receptors (Ki > 10 μM). Structurally dissimilar from SR 141716A and AM 251. Shows weak binding to both 5-HT2 (Ki = 6.4 μM) and muscarinic receptors (Ki = 2.1 μM).
分子量 | 383.4 |
公式 | C24H17NO4 |
储存 | Store at RT |
纯度 | ≥98% (HPLC) |
CAS Number | 176977-56-3 |
PubChem ID | 5311257 |
InChI Key | RYNSGDFWBJWWSZ-UHFFFAOYSA-N |
Smiles | COC1=CC=C(C=C1)C1=C(C(=O)C2=CC=C(C=C2)C#N)C2=CC=C(OC)C=C2O1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
参考文献是支持产品生物活性的出版物。
Felder et al (1998) LY320135, a novel cannabinoid CB1 receptor antagonist, unmasks coupling of the CB1 receptor to stimulation of cAMP accumulation. J.Pharmacol.Exp.Ther. 284 291 PMID: 9435190
Holland et al (1999) Cannabinoid CB1 receptors fail to cause relaxation, but couple via Gi/Go to the inhibition of adenylyl cyclase in carotid artery smooth muscle. Br.J.Pharmacol. 128 597 PMID: 10516638
Pertwee (2005) Inverse agonism and neutral antagonism at cannabinoid CB1 receptors. Life Sci. 76 1307 PMID: 15670612
关键词: LY 320135, LY 320135 supplier, Selective, CB1, receptor, antagonists, inverse, agonists, cannabinoids, Receptors, LY320135, cb1r, 2387, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 LY 320135 的部分引用包括:
Stanley et al (2015) Cannabidiol causes endothelium-dependent vasorelaxation of human mesenteric arteries via CB1 activation. J Neurosci 107 568 PMID: 26092099
Vicente-Sánchez et al (2013) HINT1 protein cooperates with cannabinoid 1 receptor to negatively regulate glutamate NMDA receptor activity. Mol Brain 6 42 PMID: 24093505
Morgan et al (2008) Modulation of network oscillatory activity and GABAergic synaptic transmission by CB1 cannabinoid receptors in the rat medial entorhinal cortex. Neural Plast 2008 808564 PMID: 19079598
Czesnik et al (2007) Cannabinoid action in the olfactory epithelium. Proc Natl Acad Sci U S A 104 2967 PMID: 17301239
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.